Target General Infomation
Target ID
T84117 (Former ID: TTDR00564)
Target Name
5-HT 1E receptor (HTR1E)
Serotonin receptor 1E; S31; 5-hydroxytryptamine receptor 1E; 5-HT1E; 5-HT-1E; 5-HT 1E
Gene Name
Target Type
Successful target
Disease [+] 1 Target-related Diseases +
1 Pituitary gland disorder [ICD-11: 5A60-5A61]
Functions as a receptor for various alkaloids and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase activity. G-protein coupled receptor for 5-hydroxytryptamine (serotonin).
BioChemical Class
GPCR rhodopsin
UniProt ID
Drugs and Modes of Action
Approved Drug(s) [+] 1 Approved Drugs +
1 Metergolin Drug Info Approved Hyperprolactinaemia [2]
Mode of Action [+] 2 Modes of Action +
Antagonist [+] 3 Antagonist drugs +
1 Metergolin Drug Info [1]
2 1-naphthylpiperazine Drug Info [1]
3 9-OH-risperidone Drug Info [5]
Agonist [+] 13 Agonist drugs +
1 2-(5-fluoro-1H-indol-3-yl)ethanamine Drug Info [1]
2 2-methyl-5-HT Drug Info [3]
3 5-BODMT Drug Info [4]
4 5-CT Drug Info [1]
5 alpha-methyl-5-HT Drug Info [1]
6 B173 Drug Info [6]
7 BRL-15572 Drug Info [7]
8 BRL54443 Drug Info [8]
9 EDMT Drug Info [9]
10 lysergol Drug Info [10]
11 m-chlorophenylpiperazine Drug Info [1]
12 TFMPP Drug Info [1]
13 [3H]5-HT Drug Info [11]
Target Affiliated Biological Pathways
KEGG Pathway [+] 3 KEGG Pathways +
1 cAMP signaling pathway
2 Neuroactive ligand-receptor interaction
3 Serotonergic synapse
Panther Pathway [+] 2 Panther Pathways +
1 Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway
2 5HT1 type receptor mediated signaling pathway
Reactome [+] 2 Reactome Pathways +
1 Serotonin receptors
2 G alpha (i) signalling events
WikiPathways [+] 5 WikiPathways +
1 Serotonin HTR1 Group and FOS Pathway
2 Monoamine GPCRs
3 GPCRs, Class A Rhodopsin-like
4 GPCR ligand binding
5 GPCR downstream signaling
REF 1 Molecular cloning and pharmacological characterization of the guinea pig 5-HT1E receptor. Eur J Pharmacol. 2004 Jan 26;484(2-3):127-39.
REF 2 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 3 Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase. Proc Natl Acad Sci U S A. 1993 Jan 15;90(2):408-12.
REF 4 Toward selective drug development for the human 5-hydroxytryptamine 1E receptor: a comparison of 5-hydroxytryptamine 1E and 1F receptor structure-affinity relationships. J Pharmacol Exp Ther. 2011 Jun;337(3):860-7.
REF 5 Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. Psychopharmacology (Berl). 1996 Mar;124(1-2):57-73.
REF 6 The gamma-aminobutyric acid-B receptor agonist baclofen attenuates responding for ethanol in ethanol-dependent rats. Alcohol Clin Exp Res. 2007 Jan;31(1):11-8.
REF 7 SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors. Naunyn Schmiedebergs Arch Pharmacol. 1997 Sep;356(3):312-20.
REF 8 Characterization of the serotonin receptor mediating contraction in the mouse thoracic aorta and signal pathway coupling. J Pharmacol Exp Ther. 2001 Apr;297(1):88-95.
REF 9 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. J Med Chem. 2000 Mar 9;43(5):1011-8.
REF 10 Two amino acid differences in the sixth transmembrane domain are partially responsible for the pharmacological differences between the 5-HT1D beta and 5-HT1E 5-hydroxytryptamine receptors. J Neurochem. 1996 Nov;67(5):2096-103.
REF 11 Molecular cloning of a serotonin receptor from human brain (5HT1E): a fifth 5HT1-like subtype. Proc Natl Acad Sci U S A. 1992 Jun 15;89(12):5517-21.

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